Emerging technologies to increase gastrointestinal transit times of drug delivery systems

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Apart from already established technologies to increase gastrointestinal transit times, including devices rapidly increasing in size once they have reached the stomach in order to retard the passage through the pylorus, formulations that float on gastric fluids and mucoadhesive drug delivery systems adhering to the gastrointestinal mucosa, there are new technologies emerging that might be game changing. They include mucus permeating nanocarriers that are able to diffuse deeply into the mucus gel layer of the gastric and intestinal mucosa remaining there for a prolonged time period (i), charge-converting nanocarriers that shift their zeta potential from negative to positive within the mucus gel layer providing strong ionic bonds with anionic mucus glycoproteins (ii) and thiolated nanocarriers and cyclodextrins form even covalent bonds with cysteine-rich subdomains of mucus glycoproteins (iii). [1]

60% of thiolated CD and only 20% of unmodified CD remained on the mucosa in rats after a four-hour period:

Distribution and remaining amount of CD in rat gastrointestinal tract for per-thiolated (red columns) and native (blue columns) β-CDs, 4 h after oral administration; (***P < 0.001, **P < 0.01); a[2].

[1] Kali, G., Knoll, P., Bernkop-Schnürch, A., Emerging technologies to increase gastrointestinal transit times of drug delivery systems. Journal of Controlled Release 346, 2022, 289-299.

[2] Kali, G., Haddadzadegan, S., Laffleur, F., Bernkop-Schnürch, A., Per-Thiolated β-Cyclodextrins: Mucoadhesive Excipients Providing a Prolonged Gastrointestinal Residence Time. http://dx.doi.org/10.2139/ssrn.4036158

[3] Grassiri B, Cesari A, Balzano F, Migone C, Kali G, Bernkop-Schnürch A, Uccello-Barretta G, Zambito Y, Piras AM. Thiolated 2-Methyl-β-Cyclodextrin as a Mucoadhesive Excipient for Poorly Soluble Drugs: Synthesis and Characterization. Polymers (Basel). 2022 Aug 3;14(15):3170. doi: 10.3390/polym14153170

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